Abstract
Recent era aims at developing safer partial Peroxisome proliferator-activated receptor-γ (PPAR- γ) agonists in order to dodge the toxicity issues related to full agonists. With a view to develop non-thiazolidinediones as partial PPAR-γ agonists, novel analogues of oxazol-5-ones (3a-3q) were designed and virtually analyzed for their molecular and drug like properties. The newly synthesized compounds were further evaluated for their preliminary cytotoxicity in a panel of eight cancer cell lines using four concentrations at 10- fold dilutions. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. All the compounds demonstrated distinct effect in the extent of cytotoxicity in the breast cancer cell line MCF-7 with 3g specifically exhibiting partial PPAR-γ agonist activity and adipogenesis stimulating ability.
Keywords: Akt/mTOR/p70S6 signalling, Cancer, Sulforhodamine B.
Anti-Cancer Agents in Medicinal Chemistry
Title:Design and Development of Oxazol-5-Ones as Potential Partial PPAR-γ Agonist Against Cancer Cell Lines
Volume: 14 Issue: 6
Author(s): Tanushree Pal, Hardik Joshi and C.S. Ramaa
Affiliation:
Keywords: Akt/mTOR/p70S6 signalling, Cancer, Sulforhodamine B.
Abstract: Recent era aims at developing safer partial Peroxisome proliferator-activated receptor-γ (PPAR- γ) agonists in order to dodge the toxicity issues related to full agonists. With a view to develop non-thiazolidinediones as partial PPAR-γ agonists, novel analogues of oxazol-5-ones (3a-3q) were designed and virtually analyzed for their molecular and drug like properties. The newly synthesized compounds were further evaluated for their preliminary cytotoxicity in a panel of eight cancer cell lines using four concentrations at 10- fold dilutions. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. All the compounds demonstrated distinct effect in the extent of cytotoxicity in the breast cancer cell line MCF-7 with 3g specifically exhibiting partial PPAR-γ agonist activity and adipogenesis stimulating ability.
Export Options
About this article
Cite this article as:
Pal Tanushree, Joshi Hardik and Ramaa C.S., Design and Development of Oxazol-5-Ones as Potential Partial PPAR-γ Agonist Against Cancer Cell Lines, Anti-Cancer Agents in Medicinal Chemistry 2014; 14 (6) . https://dx.doi.org/10.2174/1871520614666140528155118
DOI https://dx.doi.org/10.2174/1871520614666140528155118 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Advances in Nanomedicines and Targeted Therapies for Colorectal Cancer
Colorectal cancer remains a significant global health challenge, with high incidence and mortality rates despite advancements in treatment strategies. Conventional therapies often face limitations such as systemic toxicity, drug resistance, and suboptimal targeting. The advent of nanomedicines and innovative drug delivery systems offers new hope for overcoming these challenges and ...read more
Discovery of Lead compounds targeting transcriptional regulation
Transcriptional regulation plays key physiological functions in body growth and development. Transcriptional dysregulation is one of the important biomarkers of tumor genesis and progression, which is involved in regulating tumor cell processes such as cell proliferation, differentiation, and apoptosis. Additionally, it plays a pivotal role in angiogenesis and promotes tumor ...read more
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes that aid in stabilizing chromosomal makeup. The resynthesis of telomeres is supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no telomerase activity in human somatic cells, but the stem cells and germ cells undergo ...read more
Innovative targets in medicinal chemistry
Medicinal chemistry continuously evolves in response to emerging healthcare needs and advancements in scientific understanding. This special issue explores the current landscape of innovative targets in medicinal chemistry, highlighting the quest for novel therapeutic avenues. From traditional drug targets such as enzymes and receptors to emerging targets like protein-protein interactions ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Treatment of Multiple Sclerosis
CNS & Neurological Disorders - Drug Targets Genetic Variation in the β2-Adrenergic Receptor: Impact on Intermediate Cardiovascular Phenotypes
Current Pharmacogenomics and Personalized Medicine Microfilament Actin Remodeling as a Potential Target for Cancer Drug Development
Current Cancer Drug Targets The Chemical Defensive System in the Pathobiology of Idiopathic Environment- Associated Diseases
Current Drug Metabolism Intestinal Immunomodulation. Role of Regulative Peptides and Promising Pharmacological Activities
Current Pharmaceutical Design The Epigenetic Modification of Epigallocatechin Gallate (EGCG) on Cancer
Current Drug Targets Cytochrome P450 Retinoic Acid 4-Hydroxylase Inhibitors: Potential Agents for Cancer Therapy
Mini-Reviews in Medicinal Chemistry Cytotoxic Constituents from Vietnamese Marine Sponge <i>Haliclona oculata (Linnaeus, 1759)</i>
Letters in Organic Chemistry Evidence for the Involvement of Resistin in Inflammation and Cardiovascular Disease
Current Diabetes Reviews Peripheral and Central Glutamate Dyshomeostasis in Neurodegenerative Disorders
Current Neuropharmacology Glutamine, Glucose and other Fuels for Cancer
Current Pharmaceutical Design Editorial [Hot Topic: Innate Immune Responses in CNS Neurodegenerative Diseases (Guest Editors: Hans van Noort and Sandra Amor)]
CNS & Neurological Disorders - Drug Targets DNA Demethylation by TET Proteins: A Potential Therapeutic Target in Cancer
Epigenetic Diagnosis & Therapy (Discontinued) Gene Expression-Based Pharmacodynamic Biomarkers: The Beginning of a New Era in Biomarker-Driven Anti-Tumor Drug Development
Current Molecular Medicine Novel Hybrid Molecules Based on triazole-β-lactam as Potential Biological Agents
Mini-Reviews in Medicinal Chemistry Anticoagulant and Fibrinolytic Drugs – Possible Agents in Treatment of Lung Cancer?
Anti-Cancer Agents in Medicinal Chemistry The Epigenetics of Breast Carcinogenesis and Metastasis
Current Genomics Therapeutic Potential of Naturally Occurring Lignans as Anticancer Agents
Current Topics in Medicinal Chemistry Embryonic Stem Cells: Overcoming the Immunological Barriers to Cell Replacement Therapy
Current Stem Cell Research & Therapy Editorial [Hot Topic:Toward Translational Research on VIP AND PACAP (Executive Editor: A. Arimura)]
Current Pharmaceutical Design